CN104224918A - Preparation method and application of flos magnolia volatile oil microcapsules - Google Patents
Preparation method and application of flos magnolia volatile oil microcapsules Download PDFInfo
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- CN104224918A CN104224918A CN201410450740.5A CN201410450740A CN104224918A CN 104224918 A CN104224918 A CN 104224918A CN 201410450740 A CN201410450740 A CN 201410450740A CN 104224918 A CN104224918 A CN 104224918A
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Abstract
The invention relates to a preparation method and an application of flos magnolia volatile oil microcapsules. The preparation method of the microcapsules comprises the following steps: (1) fusing raw materials; (2) homogenizing at high pressure; and (3) freezing and drying to form the microcapsules. The microcapsules have relatively high water solubility and stability. Pharmacodynamic evaluation shows that the microcapsules have obvious anti-inflammatory, antiallergic and anti-asthmatic activities and can be used for preparing drugs for treating anaphylactic diseases comprising allergic asthma and allergic rhinitis.
Description
Technical field
The invention belongs to medical art, be specifically related to a kind of preparation method and application thereof of Flos Magnoliae volatile oil microcapsule.
Background technology
Flos Magnoliae is the dry flower of Magnoliacea plant Flos Magnoliae, Magnolia denudata or Flos Magnoliae, another name Flos Jasmini Nudiflori, flos magnoliae.Property and flavor of peppery and warm, returns lung meridian.There is effect of dispersing wind and cold, logical Bi Qiao, be used for the treatment of the diseases such as headche due to wind-cold, nasal obstruction, nasal sinusitis, turbid nasal discharge.The main active of Flos Magnoliae is volatile oil, comprise 1,8-eucalyptol, eugenol, methyl chavicol etc., have and significantly shrink nasal mucosa vessels and antihistaminic effect, and blood flow rate can be increased, improve microcirculation and good antiallergic and antiasthmatic effect, can as the component of the acute and chronic sinusitis for the treatment of and allergic rhinitis medicine.
Allergic rhinitis is commonly encountered diseases, the frequently-occurring disease of current nose section, and touching difficulty more.Current doctor trained in Western medicine lacks specific treatment means, and Chinese medicine life-time service Flos Magnoliae is as the principal agent of this disease for the treatment of.And determined curative effect, but traditional method has defects such as proving effective slowly, consumption is large.Antiallergic main component Flos Magnoliae volatile oil in Flos Magnoliae is made microcapsule by the present invention, and this microcapsule embedded rate is high, drug effect is good.
Microcapsule technology is a kind of a kind of resist technology adopting filmogen some to be had reactivity, sensitivity or volatile liquid or solid encapsulating formation fine particle; the process of encapsulating is micro encapsulation; the fine particle formed is called microcapsule; size is generally at 1 ~ 1000 μm, and the thickness of cyst wall is at 0.2 ~ 10 μm.The function of microcapsule mainly contains: one is the effect preventing or slow down the protection cores such as unstable core material volatilization, oxidation and corruption; Two is overcome some core material poor fluidities, not easily preserve, be inconvenient to the shortcoming of transporting; Three is bad smell or the taste of covering core material, is core material slow releasing etc. according to certain requirement.
Summary of the invention
The object of the present invention is to provide a kind of preparation method and application of Flos Magnoliae volatile oil microcapsule, this microcapsule antiallergic, asthma successful.
The present invention completes by following technical solution, and particular content comprises: the preparation method of Flos Magnoliae volatile oil microcapsule and the application in the antianaphylactic medicine of preparation.
1. a preparation method for Flos Magnoliae volatile oil microcapsule, comprises the steps:
A. be the maltodextrin of 1:2 ~ 3 and ethyl cellulose with the mass ratio of 50 ~ 60 weight portions be wall material, be dissolved in the hot water of 60 ~ 70 DEG C of described wall material weight 1 ~ 3 times, stir, obtain wall material solution;
B. be that the soybean lecithin of 1:1 ~ 2 and the blended emulsifier of sodium lauryl sulphate add in wall material solution by the mass ratio of 1 ~ 2 weight portion, mix homogeneously;
C. the last core Flos Magnoliae volatile oil by 38 ~ 49 weight portions joins in above-mentioned solution, high pressure homogenizer is passed into after 10000 ~ 12000r/min high-speed stirred 10min, homogenizing three times under 60 ~ 70 DEG C and pressure 10 ~ 20MPa, each 5min, forms the emulsion of uniform particle diameter;
D. by the emulsion after homogenizing after 0 ~ 5 DEG C of cold preservation 24h, under vacuum 0.08MPa ~ 0.10 MPa and temperature 10 ~ 25 DEG C of conditions, adopt Medium speed filter paper to filter, obtain filter cake;
E. the filter cake of gained in steps d is dry under vacuum is less than 20Pa, condenser temperature-50 ~-60 DEG C of conditions, obtain Flos Magnoliae volatile oil microcapsule.
The particle size distribution of described Flos Magnoliae volatile oil microcapsule is 1 ~ 30 μm.
2. the pharmacodynamic study of Flos Magnoliae volatile oil microcapsule prepared of the present invention.
A. histamine-acetylcholine is sprayed to draw and is breathed heavily test
Get white mice 60(body weight 192 ~ 200g) only, male and female half and half, white mice is put into bell jar one by one, spray into 2% acecoline and 1% histamine phosphate mixed liquor 15s equably, observe cause animal breath rapid, twitch and tumble time be less than the animal of 120s with the tumble time for the qualified animal of asthma.Animal qualified for asthma is divided into 5 groups at random, often organizes 10, (shake bile-fritillary falls apart to be respectively blank group (A), low dose group (B), middle dosage group (C), high dose group (D) and positive controls, E), B, C, D group gavages microcapsule, and A group gavage is to isometric(al) 0.5%CMC Na5mL/kg, and each group dosage is in table 1, once a day, continuous 7 days, 1h after last administration, drew according to said method spraying and breathes heavily, draw and breathe heavily the vapor recording mice tumble time, the results are shown in Table 1.
Table 1 Flos Magnoliae volatile oil microcapsule on medicine cause white mice asthma impact (n=10,
± S)
Note: compare with blank group
*p < 0.01
Result shows, the basic, normal, high dosage group of Flos Magnoliae volatile oil microcapsule and positive controls all have certain effect to white mice, obviously can extend the tumble time of mice, and, its effect increases with concentration and strengthens, comparatively shake bile-fritillary is loose rises appreciably for the rate elongation of middle dosage group and high dose group, its Be very effective.
B. passive cutaneous anaphylaxis test (PCA)
Get wistra rat 50, male and female half and half, body weight 190 ~ 200g, is divided into 5 groups at random, often organize 10, be respectively blank group (A), low dose group (B), middle dosage group (C), high dose group (D) and positive controls (shake bile-fritillary falls apart, E), A group is to 0.5%CMC10mL/kg, B, C, D group gives 0.2g/kg, 0.4g/kg, 0.6g/kg respectively, E group to loose 0.4 g/kg of shake bile-fritillary, once a day, continuous gastric infusion 5 days.Ridge depilation in 2 days after administration, spinal column both sides are according to center line 1.5cm, respectively get 2 points, often some interval 2cm, next day in different dilution factor (1:16:32) the rat ovaserum of depilation portion intradermal injection, 0.1mL/ point, totally 4 points, and before last administration 2h quiet note 1% Evans blue and ovalbumin 10mg/kg mixed liquor 1mL/ only, sacrificed by decapitation after 2h.Observation index: open skin of back, measures the locus coeruleus diameter that Evans blue oozes out.Calculate PCA inhibition percentage (%).PCA inhibition percentage=(blank group locus coeruleus diameter-medication group locus coeruleus diameter)/blank group locus coeruleus diameter × 100%.The results are shown in Table 2:
Impact that table 2 Flos Magnoliae volatile oil microcapsule reacts models of passive skin irritability of rats (n=10,
± S)
Note: compared with blank group,
*p < 0.01
Result shows, compared with blank group, the basic, normal, high dosage group of Flos Magnoliae volatile oil microcapsule all can show significance and suppress locus coeruleus diameter when antiserum dilution factor 1:16,1:32, show that this microcapsule has certain inhibitory action to passive anaphylaxis, its effect is fallen apart a little less than shake bile-fritillary.
Further illustrate the present invention below in conjunction with detailed description of the invention, but the scope of protection of present invention is not limited to following embodiments.
detailed description of the invention:
Embodiment 1:
The maltodextrin being 1:3 with the mass ratio of 50g and ethyl cellulose are wall material, are dissolved in the hot water of 70 DEG C of 100mL, stir, and obtain wall material solution; Be that the soybean lecithin of 1:1 and the blended emulsifier of sodium lauryl sulphate add in wall material solution by the mass ratio of 1g, mix homogeneously; Finally join in above-mentioned solution by the core Flos Magnoliae volatile oil of 49g, after 12000r/min high-speed stirred 10min, pass into high pressure homogenizer, homogenizing three times under 60 DEG C and pressure 10MPa, each 5min, forms the emulsion of uniform particle diameter; By the emulsion after homogenizing after 3 DEG C of cold preservation 24h, under vacuum 0.08MPa and temperature 25 DEG C of conditions, adopt Medium speed filter paper to filter, obtain filter cake; The filter cake of gained is dry under vacuum is less than 20Pa, condenser temperature-50 DEG C of conditions, obtain Flos Magnoliae volatile oil microcapsule.
Embodiment 2:
The maltodextrin being 1:2 with the mass ratio of 60g and ethyl cellulose are wall material, are dissolved in the hot water of 60 DEG C of 180mL, stir, and obtain wall material solution; Be that the soybean lecithin of 1:2 and the blended emulsifier of sodium lauryl sulphate add in wall material solution by the mass ratio of 2g, mix homogeneously; Finally join in above-mentioned solution by the core Flos Magnoliae volatile oil of 38g, after 10000r/min high-speed stirred 10min, pass into high pressure homogenizer, homogenizing three times under 70 DEG C and pressure 20MPa, each 5min, forms the emulsion of uniform particle diameter; By the emulsion after homogenizing after 0 DEG C of cold preservation 24h, under vacuum 0.10MPa and temperature 10 DEG C of conditions, adopt Medium speed filter paper to filter, obtain filter cake; The filter cake of gained is dry under vacuum is less than 20Pa, condenser temperature-60 DEG C of conditions, obtain Flos Magnoliae volatile oil microcapsule.
Embodiment 3:
The maltodextrin being 1:2.5 with the mass ratio of 55g and ethyl cellulose are wall material, are dissolved in the hot water of 65 DEG C of 55mL, stir, and obtain wall material solution; Be that the soybean lecithin of 1:1.5 and the blended emulsifier of sodium lauryl sulphate add in wall material solution by the mass ratio of 1.5g, mix homogeneously; Finally join in above-mentioned solution by the core Flos Magnoliae volatile oil of 43.5g, after 11000r/min high-speed stirred 10min, pass into high pressure homogenizer, homogenizing three times under 65 DEG C and pressure 15MPa, each 5min, forms the emulsion of uniform particle diameter; By the emulsion after homogenizing after 5 DEG C of cold preservation 24h, under vacuum 0.09MPa and temperature 15 DEG C of conditions, adopt Medium speed filter paper to filter, obtain filter cake; The filter cake of gained is dry under vacuum is less than 20Pa, condenser temperature-55 DEG C of conditions, obtain Flos Magnoliae volatile oil microcapsule.
Claims (4)
1. a preparation method for Flos Magnoliae volatile oil microcapsule, is characterized in that, comprises the steps:
A. be the maltodextrin of 1:2 ~ 3 and ethyl cellulose with the mass ratio of 50 ~ 60 weight portions be wall material, be dissolved in the hot water of 60 ~ 70 DEG C of described wall material weight 1 ~ 3 times, stir, obtain wall material solution;
B. be that the soybean lecithin of 1:1 ~ 2 and the blended emulsifier of sodium lauryl sulphate add in wall material solution by the mass ratio of 1 ~ 2 weight portion, mix homogeneously;
C. the last core Flos Magnoliae volatile oil by 38 ~ 49 weight portions joins in above-mentioned solution, high pressure homogenizer is passed into after 10000 ~ 12000r/min high-speed stirred 10min, homogenizing three times under 60 ~ 70 DEG C and pressure 10 ~ 20MPa, each 5min, forms the emulsion of uniform particle diameter;
D. by the emulsion after homogenizing after 0 ~ 5 DEG C of cold preservation 24h, under vacuum 0.08MPa ~ 0.10MPa and temperature 10 ~ 25 DEG C of conditions, adopt Medium speed filter paper to filter, obtain filter cake;
E. the filter cake of gained in steps d is dry under vacuum is less than 20Pa, condenser temperature-50 ~-60 DEG C of conditions, obtain Flos Magnoliae volatile oil microcapsule.
2. the Flos Magnoliae volatile oil microcapsule adopting preparation method as claimed in claim 1 obtained.
3. Flos Magnoliae volatile oil microcapsule according to claim 2, is characterized in that, the particle size distribution of described Flos Magnoliae volatile oil microcapsule is 1 ~ 30 μm.
4. the application of the microcapsule according to Claims 2 or 3 in the medicine preparing anti-allergic effects.
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